中文名 | ZD-4190 |
英文名 | ZD-4190 |
别名 | 化合物ZD-4190 |
英文别名 | ZD4190 ZD-4190 ZD 4190 4-Quinazolinamine, N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[2-(1H-1,2,3-triazol-1-yl)ethoxy]- |
CAS | 413599-62-9 |
化学式 | C19H16BrFN6O2 |
分子量 | 459.27 |
溶解度 | DMSO |
存储条件 | -20℃ |
体外研究 | ZD4190 exhibits cytotoxic activity against the tumor cells. |
体内研究 | ZD4190 (100 mg/kg, p.o.) effectively delays MDA-MB-435 tumor growth in mice. In ZD4190-treated tumors, 18F-FPPRGD2 uptake has decreased significantly relative to baseline by 26.74±8.12% (p<0.05) on day 1 and by 41.19±6.63% (p<0.01) on day 3, then has returned to baseline on day 7. Tumor uptake of 18F-FLT has also decreased on both day 1 and day 3 after initiation of ZD4190 treatment. However, ZD4190 does not significantly change 18F-FDG uptake in tumors, compared with the control group. ZD4190 (50 mg/kg, p.o.) prevents outgrowth of residual tumour in a muscle model of minimal residual carcinoma. ZD4190 (12.5-100 mg/kg, p.o.) produces a dose-dependent reduction in K(trans) in PC-3 prostate tumors. At 100 mg/kg, ZD4190 reduces K(trans) in PC-3 tumors by 31% following 2 doses and by 53% following 8 doses. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.177 ml | 10.887 ml | 21.774 ml |
5 mM | 0.435 ml | 2.177 ml | 4.355 ml |
10 mM | 0.218 ml | 1.089 ml | 2.177 ml |
5 mM | 0.044 ml | 0.218 ml | 0.435 ml |
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